A potent nonpeptide cholecystokinin antagonist selective for peripheral tissues isolated from Aspergillus alliaceus
Ray Chang(United States Military Academy), Virginia Lotti(Merck & Co., Inc., Rahway, NJ, USA (United States)), Richard L. Monaghan(Merck & Co., Inc., Rahway, NJ, USA (United States)), J Birnbaum(Merck & Co., Inc., Rahway, NJ, USA (United States)), E. O. Stapley(Merck & Co., Inc., Rahway, NJ, USA (United States)), Michael Goetz(Merck & Co., Inc., Rahway, NJ, USA (United States)), G. Albers‐Schönberg(Merck & Co., Inc., Rahway, NJ, USA (United States)), A. Patchett(Merck & Co., Inc., Rahway, NJ, USA (United States)), Jerrold M. Liesch(Merck & Co., Inc., Rahway, NJ, USA (United States)), Otto D. Hensens(Merck & Co., Inc., Rahway, NJ, USA (United States)), al. et(Merck & Co., Inc., Rahway, NJ, USA (United States))
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Abstract
A new, competitive, nonpeptide cholecystokinin (CCK) antagonist, asperlicin, was isolated from the fungus Aspergillus alliaceus. The compound has 300 to 400 times the affinity for pancreatic, ileal, and gallbladder CCK receptors than proglumide, a standard agent of this class. Moreover, asperlicin is highly selective for peripheral CCK receptors relative to brain CCK and gastrin receptors. Since asperlicin also exhibits long-lasting CCK antagonist activity in vivo, it should provide a valuable tool for investigating the physiological and pharmacological actions of CCK.
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